Multitarget AD-IN-8
Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C31H34N2O8
- Molecular Weight:562.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
BACE1 |
Bax |
Bcl-2 |
Caspase-1 |
ERK1 |
ERK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-12 | EC50 |
1.24 μM
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Neuroprotective activity against Aβ25-35-induced injury in PC12 cells assessed as increase in cell viability incubated for 24 hrs by CCK-8 assay.
Neuroprotective activity against Aβ25-35-induced injury in PC12 cells assessed as increase in cell viability incubated for 24 hrs by CCK-8 assay.
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42628381 |
In Vitro
Multitarget AD-IN-8 (Compound S12) (20 μM) demonstrates potent neuroprotective activity against Aβ25-35 induced injury in PC12 cells with an EC50 of 1.24 μM[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) suppresses the aberrant phosphorylation of tau protein at Thr181 and Ser396 in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the Aβ25-35 induced activation of the NF-κB signaling pathway in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) suppresses Aβ25-35 induced activation of the MAPK signaling pathway in PC12 cells[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the production of BACE1 in PC12 cells induced by Aβ25-35[1].
Multitarget AD-IN-8 (5-20 μM; 1 h pretreatment and 24 h Aβ25-35 exposure) inhibits the activation of the Bax/Bcl-2 pathway and suppresses caspase-1 activation in PC12 cells[1].
Multitarget AD-IN-8 (20 μM; 24 h) effectively suppresses Aβ25-35 induced apoptosis in PC12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12
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Concentration:5-20 μM
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Incubation Time:1 h (pretreatment); 24 h (Aβ25-35 exposure)
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Result:Markedly attenuated Aβ25-35 induced hyperphosphorylation of tau at Thr181 and Ser396 residues.
Inhibited the relative protein expression of p-Tau (Thr181)/Total-Tau and p-Tau (Ser396)/Total-Tau.\nAt a concentration of 20 μM, significantly attenuated Aβ25-35 induced phosphorylation of NF-κB.
Exhibited greater inhibitory activity than both donepezil and UA.\nAttenuated the Aβ25-35 induced upregulation of p-p38/p38, p-ERK1/2/ERK1/2, and p-JNK/JNK.\nMarkedly attenuated the Aβ25-35 induced BACE1 upregulation.\nAttenuated the Aβ25-35 induced upregulation of the Bax/Bcl-2 ratio and caspase-1 expression.
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Cell Line:PC12
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Concentration:20 μM
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Incubation Time:24 h
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Result:Reduced the percentage of apoptotic PC12 cells to 11%, compared to the Aβ25-35 group which had an apoptosis rate of 35.2%.
In Vivo
Multitarget AD-IN-8 (12.5-50 mg/kg; i.g.; daily; 20 consecutive days) exhibits no overt toxicity in major organs including the heart, liver, spleen, and kidneys in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (Male, 20-25 g)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:i.g.; daily; 21 consecutive days
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Result:Ameliorated the alternation behavior deficit in the Y-maze test.
Increased the discrimination index (DI) and preference index (PI) at 1 h and 24 h in the novel object recognition test.
Decreased escape latency and swimming distance in the Morris water maze, with the 50 mg/kg group differing significantly from the model group.
Increased time spent in and distance traveled within the target quadrant in the spatial probe test, with the 50 mg/kg group showing the most pronounced improvement.
Resulted in a more organized neuronal architecture and significantly attenuated neuronal damage in both the CA1 and CA3 regions.
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Animal Model:ICR mice (Male)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:i.g.; daily; 20 consecutive days
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Result:No abnormal behavior, mortality, or clinically significant changes in body weight were observed.
HE staining of major organs (heart, liver, spleen, and kidney) showed no obvious pathological lesions in all groups.
Chemical Information
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Molecular Weight 562.61
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Formula C31H34N2O8
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SMILES
CC(C1=C(O)C(C)=C(O)C([C@@]2(C)C(/C3=C(NC4=CC=C(OC(N(CCC)CCC)=O)C=C4)/C)=O)=C1OC2=CC3=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Multitarget AD-IN-8 Related Classifications
HY-189262 Related Classifications
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